IOX 2

SKU: orb1223616

Description

IOX2 is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).(In Vitro):IOX2 (0, 10, 25, and 50 μM) dose-dependently inhibits collagen-related peptide (CRP; 0.25 μg/mL) or thrombin (0.03 U/mL)-induced platelet aggregation and ATP release. But IOX2 doesn’t affect P-selectin expression and the surface levels of glycoprotein (GP)Ibα, GPVI, or αIIbβ3.IOX2 also inhibits the spreading of platelets on fibrinogen or collagen and clot retraction.IOX2 (50 μM; 24 h) increases the transcription level of VEGF-A and BNIP3 in Normal human epidermal keratinocytes (NHEK) and Normal human dermal fibroblasts (NHDF), when grown under normoxia and hypoxia condition.(In Vivo):IOX2 (10 mg/kg; i.p.; single dose) impaired the in vivo hemostatic function of platelets and arterial thrombus formation in mice.

Key Properties

• CAS Number: 931398-72-0
• MW: 352.34
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆N₂O₅
• SMILES: O=C(O)CNC(C1=C(O)C2=C(N(CC3=CC=CC=C3)C1=O)C=CC=C2)=O
• Target: HIF/HIF Prolyl-hydroxylase
• Solubility: DMSO: 7 mg/mL (19.86 mM)

Bioactivity

• In Vivo:
  Animal model: Mouse. Dosage: 10 mg/kg. Administration: Intraperitoneal injection. Result: Upregulated HIF-1α in platelets, decreased ROS generation, and downregulated NOX1 expression. Increased the phosphorylation level of VASP (Ser157/239), and inhibited the phosphorylation of p38 (Thr180/Tyr182), ERK1/2 (Thr202/Tyr204), AKT (Thr308/Ser473), and PKCδ (Thr505) in CRP-or thrombin-stimulated platelets.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IOX2 | IOX-2 | IOX 2

Quick Database Links

Gene Symbol

HIF/HIF Prolyl-hydroxylase